CirclePharma, Inc., today announced that it will apply its computational design and synthetic chemistry platform to design and create a physical screening library of novel macrocyclicpeptides. Once completed, the library is initially expected to comprise several hundred macrocycles that will be designed to potentially disrupt bioactive conformations commonly found in protein-protein interactions known to drive disease processes, and will deploy backbone scaffolds screened in silica for intrinsic cell permeability characteristics. In addition, the design of the library will permit the simple creation of derivative libraries tailored to specific features of a therapeutic target class.
PfizerInc.(NYSE:PFE) has entered into an agreement with Circle under which Pfizer will provide support for the library build, and Circle has granted Pfizer non-exclusive rights to screen the library against certaintargets. The rights granted to Pfizer exclude specified targets for which Circle has reserved exclusive rights to screen the library.
“This physical library will complement Circle’s target-specific computational design toolkit,” said David J. Earp, J.D., Ph.D., Circle’s President and CEO. “We expect to use the library for our internal pipeline discovery work, and we will make it available to all of our collaboration partners in drug discovery.”
About Macrocyclic Peptides
Macrocyclic peptides have the potential to provide access to the large proportion of therapeutic targets (estimated at up to 80%) that are considered undruggable with conventional small molecule or biologic modalities. Inparticular, there is great interest in developing macrocycles to modulate protein-protein interactions, which play a role in almost all disease conditions, including cancer, fibrosis, inflammation and infection. However, the development of macrocyclic therapeutics has been limited to this point by the need for a greater understanding of how to design macrocycles with appropriate pharm acokinetics, cell permeability and oral bioavailability. As a result, most clinical-stage macro cyclic peptide drugs address extracellular protein targets because of the challenge of identifying cell permeable macrocycles. The ability to design potent macrocycles with intrinsic permeability is expected to give access to a large number of important therapeutic targets that have been out of reach to this point.
About Circle Pharma
Founded by computational chemist Prof. Matthew Jacobson (UC San Francisco) and peptide chemist Prof. Scott Lokey (UC Santa Cruz), Circle Pharma is developing a new paradigm for macrocycle drug discovery. Circle’s technology facilitates the design and synthesis of intrinsically cell-permeable macrocycles that can address both intra- and extra-cellular therapeutic targets, and can be delivered by oral administration. Circle’s macrocycle development platform is applicable across a wide range of serious diseases; the company is initially focusing its internal development efforts on intracellular protein-protein interactions that are key drivers in cancer.
September 12, 2016, South San Francisco, CA
Circle Pharma, Inc., today announced that co-founder Prof. Matthew Jacobson has been appointed Chair of the UCSF Department of Pharmaceutical Chemistry.
“This is a terrific recognition of Matt’s exceptional accomplishments as a scientist and his passionate commitment as an educator,” said David J. Earp, JD, PhD, Circle’s President and CEO. “We are very appreciative of the guidance and leadership that our two co-founders – Matt Jacobson and Scott Lokey – continue to provide to Circle.”
Prof. Jacobson’s work at UCSF has focused on understanding the complex interactions of drugs and proteins and the implications of the underlying molecular dynamics for biology and drug discovery. In addition to his founding role in Circle, Prof. Jacobson was also a co-founder of Global Blood Therapeutics (NADAQ:GBT) and serves on the Scientific Advisory Board of Schrodinger, LLC. He has authored more that 140 publictions and has served on the editorial boards of eight journals. Prof. Jacobson joined the UCSF faculty in 2002. He earned a PhD in chemistry from the Massachusetts Institute of Technology, and did his postdoctoral work at Oxford and Columbia.
About Circle Pharma
Founded by computational chemist Prof. Matthew Jacobson (UC San Francisco) and peptide chemist Prof. Scott Lokey (UC Santa Cruz), and seed funded by Pfizer and Mission Bay Capital in 2014 and ShangPharma Investment Group Limited in 2015, Circle Pharma is developing a new paradigm for macrocycle drug discovery. Circle’s technology facilitates the design and synthesis of intrinsically cell- permeable macrocycles that can address both intra- and extra-cellular therapeutic targets, and can be delivered by oral administration. Circle’s macrocycle development platform is applicable across a wide range of serious diseases; the company is initially focusing its internal development efforts on intracellular protein-protein interactions that are key drivers in cancer.
January 19, 2016, South San Francisco
Circle Pharma, Inc., today announced that it has extended its seed funding round with an investment from ShangPharma Investment Group Limited. In conjunction with this investment, Circle has relocated to office and laboratory space in South San Francisco.
“The addition of laboratory operations to our computational chemistry platform marks the next stage of Circle’s development,” said David J. Earp, J.D., Ph.D., Circle’s President and CEO, “and we have now initiated work on Circle’s internal pipeline of macrocycle therapeutics.”
“We have selected several intracellular protein-protein interactions (“PPIs”) that play key roles in oncology as our first target group. The clinical and commercial potential of this target class is well recognized but it has proven largely intractable to small molecule drugs since these are too small to disrupt the dispersed molecular interactions typical of PPIs. And, while macrocyclic peptides are large enough to disrupt those interactions, permeability challenges – getting macrocycles into cells – have so far limited progress in this promising drug class. Circle’s ability to design intrinsically cell permeable macrocycles gives us a unique opportunity to develop first-in-class drugs against these high value drug targets.”
Working with a panel of renowned oncology experts, Circle selected its first PPI target group based on criteria including the biological validation of the target’s role as a driver of cancer, unmet clinical need and availability of structural information on the PPIs involved. This first target group includes a balance of well established targets such as PPIs in the Wnt/beta-catenin pathway, and emerging targets such as PPIs involved in epigenetic regulation.
Circle initiated operations in 2014 with seed funding from Pfizer and Mission Bay Capital. Circle deployed that first seed funding to build its computational design platform and to support its ongoing collaborative work with Pfizer. Circle’s new investor, ShangPharma Investment Group Limited, is part of the ShangPharma Group which includes the full service CRO ChemPartner. Circle will work with ChemPartner to build physical libraries of conformationally diverse, cell permeable macrocycles which Circle will integrate into its macrocycle drug development platform.
About Macrocyclic Peptides
Macrocyclic peptides have the potential to provide access to the large proportion of therapeutic targets (estimated at up to 80%) that are considered undruggable with conventional small molecule or biologic modalities. In particular, there is great interest in developing macrocycles to modulate protein-protein interactions, which play a role in almost all disease conditions, including cancer, fibrosis, inflammation and infection. However, the development of macrocyclic therapeutics has been limited to this point by the need for a greater understanding of how to design macrocycles with appropriate pharmacokinetics, cell permeability and oral bioavailability. As a result, most clinical-stage macrocyclic peptide drugs address extracellular protein targets because of the challenge of identifying cell permeable macrocycles. The ability to design potent macrocycles with intrinsic permeability is expected to give access to a large number of important therapeutic targets that have been out of reach to this point.
About Circle Pharma
Founded by computational chemist Prof. Matthew Jacobson (UC San Francisco) and peptide chemist Prof. Scott Lokey (UC Santa Cruz), and seed funded by Pfizer and Mission Bay Capital in 2014, Circle Pharma is developing a new paradigm for macrocycle drug discovery. Circle’s technology facilitates the design and synthesis of intrinsically cell-permeable macrocycles that can address both intra- and extra- cellular therapeutic targets, and can be delivered by oral administration. Circle’s macrocycle development platform is applicable across a wide range of serious diseases; the company is initially focusing its internal development efforts on intracellular protein-protein interactions that are key drivers in cancer.
January 7, 2016, South San Francisco
Circle Pharma, Inc., a newly created, early-stage biotechnology company, today announced that it has received seed funding from Pfizer Inc. and QB3’s seed-stage venture fund, Mission Bay Capital, LLC, and has initiated two collaborations with Pfizer to develop cell permeable macrocyclic peptide therapeutics.
“We are very pleased to have launched Circle with the backing of Pfizer and Mission Bay Capital, and to have initiated two exciting collaborative projects with Pfizer,” said David J. Earp, J.D., Ph.D., Circle’s President and CEO. “In addition to these collaborations, Circle will be undertaking development work against our own therapeutic targets. We are open to additional collaborations with partners who share our excitement in the potential of permeable macrocyclic peptides, which, we believe, could be applicable to a large number of important therapeutic targets.”
Circle’s technology is based in part on research sponsored by Pfizer through an agreement with QB3.
About Macrocyclic Peptides
Macrocyclic peptides have the potential to provide access to therapeutic targets that are considered undruggable with conventional small molecule or biologic modalities. In particular, there is great interest in developing macrocycles to modulate protein-protein interactions, which play a role in almost all disease conditions, including cancer, fibrosis, inflammation and infection. However, the development of macrocyclic therapeutics has been limited to this point by the need for a greater understanding of how to design macrocycles with appropriate pharmacokinetics, cell permeability and oral bioavailability. Indeed, today, most clinical programs testing macrocyclic peptides are aimed at extracellular protein targets because of the challenge of identifying cell permeable macrocycles. The ability to design potent macrocycles with inherent permeability is expected to give access to a large number of important therapeutic targets that have been out of reach to this point.
About Circle
Circle Pharma is an early stage biotechnology company applying proprietary computational design algorithms and innovative chemistry to develop cell permeable macrocycle peptide therapeutics against important clinical targets. It does this through an iterative, rational design process that deploys large virtual libraries of conformationally diverse macrocycle scaffolds selected for inherent permeability. The company was founded by Prof. Matt Jacobson, Ph.D. (U.C. San Francisco) and Prof. Scott Lokey, Ph.D. (U.C. Santa Cruz) and is headed by David J. Earp, J.D., Ph.D.
September 22, 2014, San Francisco